Patent SG-11201810138X-A (SG)
Title: Beta-hairpin peptidomimetic with elastase inhibitory activity and aerosol dosage forms thereof
Inventor: BRUIJNZEEL PIET
IPC: C07K7/64
Filed: 2017-05-31
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 11111111111111111111011111 110 11E111110 11111111111111111111110 11111111111 Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\"\" WO 2017/207118 Al 07 December 2017 (07.12.2017) WIP0 I PCT (51) International Patent Classification: DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, A61K 8/64 (2006.01) A61P 11/00 (2006.01) HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, A61K 38/12 (2006.01) CO7K 7/64 (2006.01) KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, A61K 9/00 (2006.01) MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, (21) International Application Number: PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, PCT/EP2017/025157 SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (22) International Filing Date: (84) Designated States (unless otherwise indicated, for every 31 May 2017 (31.05.2017) kind of regional protection available): ARIPO (BW, GH, (25) Filing Language: English GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, (26) Publication Language: English UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (30) Priority Data: EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, 16020210.7 31 May 2016 (31.05.2016) EP MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, (71) Applicant: POLYPHOR AG [CH/CH]; Hegenheimermat- KM, ML, MR, NE, SN, TD, TG). tweg 125, 4123 Allschwil (CH). (72) Inventors: BRUIJNZEEL, Piet; Wim Sonneveldlaan Published: 241, 3584 ZS Utrecht (NL). ZIMMERMANN, Jo- — with international search report (Art. 21(3)) _ Kann; Konigsberger Strasse 9, 79379 Mullheim (DE). BARTH, Philip; Bernoullistrasse 10, 4056 Basel (CH). CHEVALIER, Eric; 10 rue de l'ecole, 68440 Stein- = - brunn-le-bas (FR). LUDIN, Christian; Im Drissel 24, 4104 Oberwil (CH). KELLER, Manfred; Neunkirchner Str. 60, =_ 81379 Miinchen (DE). = = (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, = CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, Title: BETA-HAIRPIN PEPTIDOMIMETIC WITH ELASTASE INHIBITORY ACTIVITY AND AEROSOL DOSAGE FOR- = (54) = MS THEREOF = = (57) : The present invention relates to pharma- = Fig. 1 ceutical aerosols comprising a 0-hairpin peptidomimetic 0.3 of formula cyclo(-OctG-Glu-Thr-Ala-Ser-lle-Pro-Pro-Gln-Lys- = _ _ Tyr- D Pro-Pro-), or a pharmaceutically acceptable salt there- of, having inhibitory activity against human neutrophil elas- tase. It further relates to solid or liquid pharmaceutical compo- = = - = * **** sitions and kits for preparing and administering such aerosols. au **** _i .„ The invention can be used for the prevention, management or treatment of pulmonary diseases, such as alpha-1 antitrypsin deficiency (AATD), cystic fibrosis (CF), non-cystic fibrosis ..., bronchiactasis (NCFB), or chronic obstructive pulmonary dis- ease (COPD), or infections, or diseases, or conditions of the lungs, being mediated by or resulting from human neutrophil elastase activity. Thus, the invention further relates to a phar- maceutical composition or a pharmaceutical aerosol comprising = — 1-1 GC 1-1 w m the active compound cyclo(-OctG-Glu-Thr-Ala-Ser-lle-Pro-Pro- IN 0 ei IN Gln-Lys-Tyr- D Pro -Pro -), or any pharmaceutically acceptable salt thereof, for use in a method for the prevention, management or treatment of diseases or conditions of the lungs being mediated by 1-1 Inhalation dosing or resulting from human neutrophil elastase activity in a subject. 0 ei C